Granted Patent
B2
US 12,667,557 · App. 16/485,777 · Granted Jun 30, 2026
Method for treating EGFR-TKI-resistant non-small cell lung cancer by administration of anti-HER3 antibody-drug conjugate
Inventors:
Kimio Yonesaka (Osaka-Sayama, JP); Kazuhiko Nakagawa (Osaka-Sayama, JP); Kenji Hirotani (Tokyo, JP)
Assignee:
DAIICHI SANKYO COMPANY, LIMITED
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Abstract
[Problem] To provide a therapeutic agent and a therapeutic method for EGFR-TKI-resistant non-small cell lung cancer. [Solution] Provided are: a therapeutic agent that contains an anti-HER3 antibody-drug conjugate as an active ingredient, or a therapeutic method characterized by administering an anti-HER3 antibody-drug conjugate.
Claims (23)
1 . A therapeutic method for osimertinib-resistant non-small cell lung cancer, comprising administering an anti-HER3 antibody-drug conjugate to a human subject in need thereof.
2 . The therapeutic method according to claim 1 , wherein the non-small cell lung cancer is EGFR T790M mutation-negative non-small cell lung cancer.
3 . The therapeutic method according to claim 2 , wherein the osimertinib-resistant non-small cell lung cancer is further resistant to gefitinib, erlotinib or afatinib.
4 . The therapeutic method according to claim 2 , wherein the osimertinib-resistant non-small cell lung cancer is further resistant to gefitinib or erlotinib.
5 . The therapeutic method according to claim 1 , wherein the osimertinib-resistant non-small cell lung cancer is further resistant to gefitinib, erlotinib, afatinib, or a combination thereof.
6 . The therapeutic method according to claim 1 , wherein the non-small cell lung cancer expresses HER3.
7 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody-drug conjugate is an anti-HER3 antibody-drug conjugate in which a drug-linker represented by the following formula:
wherein A represents the connecting position to an anti-HER3 antibody,
is conjugated to the anti-HER3 antibody via a thioether bond.
8 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody is an antibody comprising a heavy chain comprising CDRH1 consisting of the amino acid sequence represented by SEQ ID NO:1, CDRH2 consisting of the amino acid sequence represented by SEQ ID NO:2, and CDRH3 consisting of the amino acid sequence represented by SEQ ID NO:3, and a light chain comprising CDRL1 consisting of the amino acid sequence represented by SEQ ID NO:4, CDRL2 consisting of the amino acid sequence represented by SEQ ID NO:5, and CDRL3 consisting of the amino acid sequence represented by SEQ ID NO:6.
9 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody is an antibody comprising a heavy chain comprising a heavy chain variable region consisting of the amino acid sequence represented by SEQ ID NO:7, and a light chain comprising a light chain variable region consisting of the amino acid sequence represented by SEQ ID NO:8.
10 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody is an antibody comprising a heavy chain consisting of the amino acid sequence represented by SEQ ID NO:9, and a light chain consisting of the amino acid sequence represented by SEQ ID NO:10.
11 . The therapeutic method according to claim 10 , wherein the anti-HER3 antibody lacks a lysine residue at the carboxyl terminus of the heavy chain.
12 . The therapeutic method according to claim 1 , wherein the average number of units of the drug-linker conjugated per antibody molecule in the anti-HER3 antibody-drug conjugate is in the range of 7 to 8.
13 . The therapeutic method according to claim 1 , wherein the average number of units of the drug-linker conjugated per antibody molecule in the anti-HER3 antibody-drug conjugate is in the range of 7.5 to 8.
14 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody-drug conjugate is administered in combination with a second drug.
15 . The therapeutic method according to claim 14 , wherein the second drug is gefitinib, erlotinib, afatinib, or osimertinib.
16 . The therapeutic method according to claim 15 , wherein the second drug is erlotinib.
17 . The therapeutic method according to claim 15 , wherein the second drug is osimertinib.
18 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody-drug conjugate comprises a drug-linker conjugated to an antibody via a thioether bond, wherein the antibody-drug conjugate releases a drug having a structure of:
19 . The therapeutic method according to claim 18 , wherein the anti-HER3 antibody-drug conjugate is administered in combination with a second drug.
20 . The therapeutic method according to claim 19 , wherein the second drug is gefitinib, erlotinib, afatinib, or osimertinib.
21 . The therapeutic method according to claim 20 , wherein the second drug is osimertinib.
Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Jul 9, 2021
From: KINKI UNIVERSITY
To: DAIICHI SANKYO COMPANY, LIMITED
Reel/Frame 056798/0735 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Aug 13, 2019
From: YONESAKA, KIMIO; NAKAGAWA, KAZUHIKO; HIROTANI, KENJI
To: KINKI UNIVERSITY; DAIICHI SANKYO COMPANY, LIMITED
Reel/Frame 050043/0400 →
Priority Claims (2)
JP 2017-035919
· Feb 28, 2017
· national
JP 2017-199883
· Oct 13, 2017
· national
Continuity (1)
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Office Action issued in corresponding Singaporean Patent Application No. 11201907050P dated Apr. 1, 2024 (9 pages).
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Office Action issued in corresponding Japanese Patent Application No. 2022-157622 dated Oct. 3, 2023 (6 pages).
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Office Action issued in corresponding Taiwanese Patent Application No. 107106568 dated Oct. 11, 2023 (20 pages).
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